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RSS FeedsMarine Drugs, Vol. 18, Pages 112: Investigating the Antiparasitic Potential of the Marine Sesquiterpene Avarone, Its Reduced form Avarol, and the Novel Semisynthetic Thiazinoquinone Analogue Thiazoavarone (Marine Drugs)

 
 

14 february 2020 16:02:53

 
Marine Drugs, Vol. 18, Pages 112: Investigating the Antiparasitic Potential of the Marine Sesquiterpene Avarone, Its Reduced form Avarol, and the Novel Semisynthetic Thiazinoquinone Analogue Thiazoavarone (Marine Drugs)
 




The chemical analysis of the sponge Dysidea avara afforded the known sesquiterpene quinone avarone, along with its reduced form avarol. To further explore the role of the thiazinoquinone scaffold as an antiplasmodial, antileishmanial and antischistosomal agent, we converted the quinone avarone into the thiazinoquinone derivative thiazoavarone. The semisynthetic compound, as well as the natural metabolites avarone and avarol, were pharmacologically investigated in order to assess their antiparasitic properties against sexual and asexual stages of Plasmodium falciparum, larval and adult developmental stages of Schistosoma mansoni (eggs included), and also against promastigotes and amastigotes of Leishmania infantum and Leishmania tropica. Furthermore, in depth computational studies including density functional theory (DFT) calculations were performed. A toxic semiquinone radical species which can be produced starting both from quinone- and hydroquinone-based compounds could mediate the anti-parasitic effects of the tested compounds.


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22 viewsCategory: Biochemistry, Molecular Biology, Pharmacology
 
Marine Drugs, Vol. 18, Pages 109: Identification of Prostaglandin Pathway in Dinoflagellates by Transcriptome Data Mining (Marine Drugs)
Marine Drugs, Vol. 18, Pages 111: The Marine-Derived Triterpenoid Frondoside A Inhibits Thrombus Formation (Marine Drugs)
 
 
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